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Synthesis of [14C]-and [3H]-labelled ICI 162,846

โœ Scribed by JR Harding; JA Bergin; DM Mant; J McCormick

Publisher
Elsevier Science
Year
1988
Weight
39 KB
Volume
39
Category
Article
ISSN
0883-2889

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โœฆ Synopsis

ICI 185,282 ((SZ)-7-[(2RS, 4RS, 5SR)-4-o-Wdroxypheny1-Ztri fluoromethyl--1,3-d|~-'an-5--yl ]-~--hepteno|c acid), a novel thromboxane receptor antagonist, has been radiolabelled with 14C for use in metabolism studies. [14C]-ICI 185,282 (1), specific activity 23.8 mCi/mmol, radiochemical purity 98% was prepared from [2,3-]4C2]succ|nic anhydride in a ten stage process in 4.1% overall radiochemical yield. H | Q O~----/~/~CO.H (x) " denotes position of 14C-]abe] SYNTHESIS OF [14C]-AND [3H]-LABELLED ICl 162,846

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โœ D. Hesk; C. Bowlen; S. Hendershot; D. Koharski; P. McNamara; D. Rettig; S. Saluj ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› John Wiley and Sons ๐ŸŒ French โš– 404 KB ๐Ÿ‘ 1 views

3H-Sch 47949, racemic 3H-Sch 48461, was prepared at a specific activity of 40 mCi/mmole by Pt catalysed exchange with tritiated water. 3H-Sch 48461 was prepared at a specific activity of 64.6 Ci/mmole by a Pd/C catalysed reduction of an olefinic intermediate. 14C-Sch 48461 was prepared in 8 steps fr